JP2016529315A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016529315A5 JP2016529315A5 JP2016540405A JP2016540405A JP2016529315A5 JP 2016529315 A5 JP2016529315 A5 JP 2016529315A5 JP 2016540405 A JP2016540405 A JP 2016540405A JP 2016540405 A JP2016540405 A JP 2016540405A JP 2016529315 A5 JP2016529315 A5 JP 2016529315A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrocarbyl
- pharmaceutical composition
- halo
- optionally substituted
- cyano
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 37
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 37
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- 125000005843 halogen group Chemical group 0.000 claims 28
- 125000004093 cyano group Chemical group *C#N 0.000 claims 26
- 238000006467 substitution reaction Methods 0.000 claims 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 208000004296 Neuralgia Diseases 0.000 claims 5
- RAXXELZNTBOGNW-UHFFFAOYSA-N Imidazole Chemical compound C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 4
- 208000002193 Pain Diseases 0.000 claims 4
- 125000004432 carbon atoms Chemical group C* 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000011780 sodium chloride Substances 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 206010001897 Alzheimer's disease Diseases 0.000 claims 2
- 206010004938 Bipolar disease Diseases 0.000 claims 2
- 208000001636 Diabetic Neuropathy Diseases 0.000 claims 2
- 206010012680 Diabetic neuropathy Diseases 0.000 claims 2
- 208000001640 Fibromyalgia Diseases 0.000 claims 2
- 206010061536 Parkinson's disease Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 230000001404 mediated Effects 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 101710035825 PRKAA1 Proteins 0.000 claims 1
- 208000001293 Peripheral Nervous System Disease Diseases 0.000 claims 1
- 206010034606 Peripheral neuropathy Diseases 0.000 claims 1
- 102000030951 Phosphotransferases Human genes 0.000 claims 1
- 108091000081 Phosphotransferases Proteins 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000002093 peripheral Effects 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 0 *N(C=CC(c(cc[n]1nc2)nc1c2-c1cccnc1)=C1)C1=O Chemical compound *N(C=CC(c(cc[n]1nc2)nc1c2-c1cccnc1)=C1)C1=O 0.000 description 2
Claims (52)
（式中、
Ｒ１はＲ１Ａ又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のＲ１Ａによるものであり、
各Ｒ１Ａは独立して、−ＯＲ１Ｃ、−Ｎ（Ｒ１Ｃ）２、−Ｃ（Ｏ）Ｒ１Ｃ、−Ｃ（Ｏ）ＯＲ１Ｃ、−Ｃ（Ｏ）Ｎ（Ｒ１Ｃ）２、−Ｎ（Ｒ１Ｃ）Ｃ（Ｏ）ＯＲ１Ｃ、シアノ、ハロ、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のＲ１Ｂによるものであり、
各Ｒ１Ｂは独立して、−ＯＲ１Ｃ、−Ｎ（Ｒ１Ｃ）２、−Ｃ（Ｏ）Ｒ１Ｃ、−Ｃ（Ｏ）ＯＲ１Ｃ、−Ｃ（Ｏ）Ｎ（Ｒ１Ｃ）２、−Ｎ（Ｒ１Ｃ）Ｃ（Ｏ）ＯＲ１Ｃ、シアノ又はハロであり、
各Ｒ１Ｃは独立して、水素、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のシアノ、ハロ又はヒドロキシルによるものであり、
Ｒ２は、炭素原子の１つがＣ５に結合した、任意に置換されたＣ１〜１２ヒドロカルビル又は２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のＲ２Ｃによるものであり、
各Ｒ２Ｃは独立して、−ＯＲ２Ｄ、−Ｎ（Ｒ２Ｄ）２、−Ｃ（Ｏ）Ｒ２Ｄ、−Ｃ（Ｏ）ＯＲ２Ｄ、−Ｃ（Ｏ）Ｎ（Ｒ２Ｄ）２、−Ｎ（Ｒ２Ｄ）Ｃ（Ｏ）ＯＲ２Ｄ、シアノ、ハロ、オキソ、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のアミノ、シアノ、ハロ、ヒドロキシル又はＲ２Ｄによるものであり、
各Ｒ２Ｄは独立して、水素、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のアミノ、シアノ、ハロ、又はヒドロキシルによるものであり、
Ｒ３は水素、又は１つ若しくは複数のシアノ、ハロ若しくはヒドロキシルで任意に置換されたＣ１〜６アルキルである）又はその薬学的に許容可能な塩に接触させることを含む、アダプター関連キナーゼ１（ＡＡＫ１）阻害剤。 Under following formula of the compound:
(Where
R 1 is R 1A or an optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is by one or more R 1A ,
Each R 1A is independently —OR 1C , —N (R 1C ) 2 , —C (O) R 1C , —C (O) OR 1C , —C (O) N (R 1C ) 2 , —N (R 1C ) C (O) OR 1C , cyano, halo, or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where optional substitution is by one or more R 1B And
Each R 1B is independently —OR 1C , —N (R 1C ) 2 , —C (O) R 1C , —C (O) OR 1C , —C (O) N (R 1C ) 2 , —N (R 1C ) C (O) OR 1C , cyano or halo,
Each R 1C is independently hydrogen, or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is by one or more cyano, halo, or hydroxyl ,
R 2 is an optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl in which one of the carbon atoms is bonded to C 5, where the optional substitution is by one or more R 2C ,
Each R 2C is independently —OR 2D , —N (R 2D ) 2 , —C (O) R 2D , —C (O) OR 2D , —C (O) N (R 2D ) 2 , —N (R 2D ) C (O) OR 2D , cyano, halo, oxo, or an optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is one or more amino, By cyano, halo, hydroxyl or R 2D ,
Each R 2D is independently hydrogen, or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where optional substitution is by one or more amino, cyano, halo, or hydroxyl Is,
R 3 is hydrogen or C 1-6 alkyl optionally substituted with one or more cyano, halo or hydroxyl) or a pharmaceutically acceptable salt thereof, adapter-related kinase 1 (AAK1) inhibitor .
（式中、
Ｒ１はＲ１Ａ又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のＲ１Ａによるものであり、
各Ｒ１Ａは独立して、−ＯＲ１Ｃ、−Ｎ（Ｒ１Ｃ）２、−Ｃ（Ｏ）Ｒ１Ｃ、−Ｃ（Ｏ）ＯＲ１Ｃ、−Ｃ（Ｏ）Ｎ（Ｒ１Ｃ）２、−Ｎ（Ｒ１Ｃ）Ｃ（Ｏ）ＯＲ１Ｃ、シアノ、ハロ、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のＲ１Ｂによるものであり、
各Ｒ１Ｂは独立して、−ＯＲ１Ｃ、−Ｎ（Ｒ１Ｃ）２、−Ｃ（Ｏ）Ｒ１Ｃ、−Ｃ（Ｏ）ＯＲ１Ｃ、−Ｃ（Ｏ）Ｎ（Ｒ１Ｃ）２、−Ｎ（Ｒ１Ｃ）Ｃ（Ｏ）ＯＲ１Ｃ、シアノ又はハロであり、
各Ｒ１Ｃは独立して、水素、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のシアノ、ハロ又はヒドロキシルによるものであり、
Ｒ２は、炭素原子の１つがＣ５に結合した、任意に置換されたＣ１〜１２ヒドロカルビル又は２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のＲ２Ｃによるものであり、
各Ｒ２Ｃは独立して、−ＯＲ２Ｄ、−Ｎ（Ｒ２Ｄ）２、−Ｃ（Ｏ）Ｒ２Ｄ、−Ｃ（Ｏ）ＯＲ２Ｄ、−Ｃ（Ｏ）Ｎ（Ｒ２Ｄ）２、−Ｎ（Ｒ２Ｄ）Ｃ（Ｏ）ＯＲ２Ｄ、シアノ、ハロ、オキソ、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のアミノ、シアノ、ハロ、ヒドロキシル又はＲ２Ｄによるものであり、
各Ｒ２Ｄは独立して、水素、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のアミノ、シアノ、ハロ、又はヒドロキシルによるものであり、
Ｒ３は水素、又は１つ若しくは複数のシアノ、ハロ若しくはヒドロキシルで任意に置換されたＣ１〜６アルキルである）又はその薬学的に許容可能な塩を含む、
ＡＡＫ１活性によって媒介される疾患又は障害を治療又は管理するための医薬組成物。 Under following formula of the compound:
(Where
R 1 is R 1A or an optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is by one or more R 1A ,
Each R 1A is independently —OR 1C , —N (R 1C ) 2 , —C (O) R 1C , —C (O) OR 1C , —C (O) N (R 1C ) 2 , —N (R 1C ) C (O) OR 1C , cyano, halo, or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where optional substitution is by one or more R 1B And
Each R 1B is independently —OR 1C , —N (R 1C ) 2 , —C (O) R 1C , —C (O) OR 1C , —C (O) N (R 1C ) 2 , —N (R 1C ) C (O) OR 1C , cyano or halo,
Each R 1C is independently hydrogen, or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is by one or more cyano, halo, or hydroxyl ,
R 2 is an optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl in which one of the carbon atoms is bonded to C 5, where the optional substitution is by one or more R 2C ,
Each R 2C is independently —OR 2D , —N (R 2D ) 2 , —C (O) R 2D , —C (O) OR 2D , —C (O) N (R 2D ) 2 , —N (R 2D ) C (O) OR 2D , cyano, halo, oxo, or an optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is one or more amino, By cyano, halo, hydroxyl or R 2D ,
Each R 2D is independently hydrogen, or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where optional substitution is by one or more amino, cyano, halo, or hydroxyl Is,
R 3 is hydrogen or C 1-6 alkyl optionally substituted with one or more cyano, halo, or hydroxyl) or a pharmaceutically acceptable salt thereof ,
A pharmaceutical composition for treating or managing a disease or disorder mediated by AAK1 activity .
（式中、
Ａは環状Ｃ１〜１２ヒドロカルビル又は４員〜７員の複素環であり、
Ｄは炭素原子の１つがＣ５に結合した、環状Ｃ１〜１２ヒドロカルビル又は４員〜７員の複素環であり、
ｎは１〜３であり、
ｍは０〜３である）又はその薬学的に許容可能な塩である、請求項２に記載の医薬組成物。 The compound is of the formula:
(Where
A is a cyclic C 1-12 hydrocarbyl or a 4-7 membered heterocycle,
D is a cyclic C 1-12 hydrocarbyl or 4-7 membered heterocycle, one of the carbon atoms bonded to C5;
n is 1 to 3,
The pharmaceutical composition according to claim 2 , wherein m is 0 to 3) or a pharmaceutically acceptable salt thereof .
（式中、
Ａは環状Ｃ１〜１２ヒドロカルビル又は４員〜７員の複素環であり、
Ｄは炭素原子の１つがＣ５に結合した、環状Ｃ１〜１２ヒドロカルビル又は４員〜７員の複素環であり、
各Ｒ１Ａは独立して、−ＯＲ１Ｃ、−Ｎ（Ｒ１Ｃ）２、−Ｃ（Ｏ）Ｒ１Ｃ、−Ｃ（Ｏ）ＯＲ１Ｃ、−Ｃ（Ｏ）Ｎ（Ｒ１Ｃ）２、−Ｎ（Ｒ１Ｃ）Ｃ（Ｏ）ＯＲ１Ｃ、シアノ、ハロ、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のＲ１Ｂによるものであり、
各Ｒ１Ｂは独立して、−ＯＲ１Ｃ、−Ｎ（Ｒ１Ｃ）２、−Ｃ（Ｏ）Ｒ１Ｃ、−Ｃ（Ｏ）ＯＲ１Ｃ、−Ｃ（Ｏ）Ｎ（Ｒ１Ｃ）２、−Ｎ（Ｒ１Ｃ）Ｃ（Ｏ）ＯＲ１Ｃ、シアノ又はハロであり、
各Ｒ１Ｃは独立して、水素、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のシアノ、ハロ又はヒドロキシルによるものであり、
各Ｒ２Ｃは独立して、−ＯＲ２Ｄ、−Ｎ（Ｒ２Ｄ）２、−Ｃ（Ｏ）Ｒ２Ｄ、−Ｃ（Ｏ）ＯＲ２Ｄ、−Ｃ（Ｏ）Ｎ（Ｒ２Ｄ）２、−Ｎ（Ｒ２Ｄ）Ｃ（Ｏ）ＯＲ２Ｄ、シアノ、ハロ、オキソ、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のアミノ、シアノ、ハロ、ヒドロキシル又はＲ２Ｄによるものであり、
各Ｒ２Ｄは独立して、水素、又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のアミノ、シアノ、ハロ、ヒドロキシルによるものであり、
ｎは１〜３であり、
ｍは０〜３である）又はその薬学的に許容可能な塩。 Compounds of the following formula:
(Where
A is a cyclic C 1-12 hydrocarbyl or a 4-7 membered heterocycle,
D is a cyclic C 1-12 hydrocarbyl or 4-7 membered heterocycle, one of the carbon atoms bonded to C5;
Each R 1A is independently —OR 1C , —N (R 1C ) 2 , —C (O) R 1C , —C (O) OR 1C , —C (O) N (R 1C ) 2 , —N (R 1C ) C (O) OR 1C , cyano, halo, or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where optional substitution is by one or more R 1B And
Each R 1B is independently —OR 1C , —N (R 1C ) 2 , —C (O) R 1C , —C (O) OR 1C , —C (O) N (R 1C ) 2 , —N (R 1C ) C (O) OR 1C , cyano or halo,
Each R 1C is independently hydrogen, or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is by one or more cyano, halo, or hydroxyl ,
Each R 2C is independently —OR 2D , —N (R 2D ) 2 , —C (O) R 2D , —C (O) OR 2D , —C (O) N (R 2D ) 2 , —N (R 2D ) C (O) OR 2D , cyano, halo, oxo, or an optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is one or more amino, By cyano, halo, hydroxyl or R 2D ,
Each R 2D is independently hydrogen, or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where optional substitution is by one or more amino, cyano, halo, hydroxyl And
n is 1 to 3,
m is 0-3) or a pharmaceutically acceptable salt thereof.
（式中、ＸはＣＨ又はＮである）である、請求項２５に記載の化合物。 Compounds of the following formula:
26. The compound of claim 25, wherein X is CH or N.
である、請求項３０に記載の化合物。 Compounds of the following formula:
32. The compound of claim 30, wherein
（式中、
Ｒ２Ｃは−Ｃ（Ｏ）Ｒ２Ｄ、−Ｃ（Ｏ）ＯＲ２Ｄ又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のアミノ、シアノ、ハロ、ヒドロキシル又はＲ２Ｄによるものである）である、請求項３０に記載の化合物。 Compounds of the following formula:
(Where
R 2C is —C (O) R 2D , —C (O) OR 2D or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is one or more amino 32. The compound of claim 30, wherein said compound is from cyano, cyano, halo, hydroxyl or R2D .
である、請求項３０に記載の化合物。 Compounds of the following formula:
32. The compound of claim 30, wherein
（式中、
Ｒ２Ｃは−Ｃ（Ｏ）Ｒ２Ｄ、−Ｃ（Ｏ）ＯＲ２Ｄ又は任意に置換されたＣ１〜１２ヒドロカルビル若しくは２員〜１２員のヘテロカルビルであり、任意の置換は１つ又は複数のアミノ、シアノ、ハロ、ヒドロキシル又はＲ２Ｄによるものである）である、請求項３０に記載の化合物。 Compounds of the following formula:
(Where
R 2C is —C (O) R 2D , —C (O) OR 2D or optionally substituted C 1-12 hydrocarbyl or 2-12 membered heterocarbyl, where the optional substitution is one or more amino 32. The compound of claim 30, wherein said compound is from cyano, cyano, halo, hydroxyl or R2D .
である、請求項３４に記載の化合物。 Compounds of the following formula:
35. The compound of claim 34, wherein
である、請求項３６に記載の化合物。 Compounds of the following formula:
37. The compound of claim 36, wherein
である、請求項３７に記載の化合物。 Compounds of the following formula:
38. The compound of claim 37, wherein
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361874395P | 2013-09-06 | 2013-09-06 | |
| US61/874,395 | 2013-09-06 | ||
| PCT/US2014/054209 WO2015035117A1 (en) | 2013-09-06 | 2014-09-05 | PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016529315A JP2016529315A (en) | 2016-09-23 |
| JP2016529315A5 true JP2016529315A5 (en) | 2017-10-05 |
| JP6472450B2 JP6472450B2 (en) | 2019-02-20 |
Family
ID=51542502
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016540405A Active JP6472450B2 (en) | 2013-09-06 | 2014-09-05 | Pyrazolo [1,5-a] pyrimidine compounds, compositions containing them, and methods of using them |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20150175610A1 (en) |
| EP (1) | EP3041475A1 (en) |
| JP (1) | JP6472450B2 (en) |
| CN (1) | CN105517553B (en) |
| AR (1) | AR097545A1 (en) |
| AU (1) | AU2014315113B2 (en) |
| CA (1) | CA2923317C (en) |
| HK (1) | HK1217658A1 (en) |
| TW (1) | TW201542550A (en) |
| WO (1) | WO2015035117A1 (en) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9737542B2 (en) | 2013-10-11 | 2017-08-22 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| EP3215510B1 (en) | 2014-11-06 | 2023-06-07 | Bial-R&D Investments, S.A. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| AU2015342883B2 (en) | 2014-11-06 | 2020-07-02 | Bial - R&D Investments, S.A. | Substituted pyrrolo(1,2-a)pyrimidines and their use in the treatment of medical disorders |
| CN115925711A (en) | 2014-11-06 | 2023-04-07 | Bial研发投资股份有限公司 | Substituted pyrazolo [1,5-a ] pyrimidines and their use in treating medical disorders |
| CA3020305A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| MX2018012207A (en) | 2016-04-06 | 2019-03-28 | Lysosomal Therapeutics Inc | Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders. |
| KR20180133461A (en) | 2016-04-06 | 2018-12-14 | 리소소말 테라퓨틱스 인크. | Pyrazolo [1,5-a] pyrimidinylcarboxamide compounds and their use in the treatment of medical disorders |
| EP3452455A4 (en) | 2016-05-05 | 2019-11-13 | Lysosomal Therapeutics Inc. | Substituted imdazo[1,2- ]pyridines, substituted imidazo[1,2- ]pyrazines, related compounds, and their use in the treatment of medical disorders |
| US11168087B2 (en) | 2016-05-05 | 2021-11-09 | Bial—R&D Investments, S.A. | Substituted imidazo[1,2-b]pyridazines, substituted imidazo[1,5-b]pyridazines, related compounds, and their use in the treatment of medical disorders |
| AU2019360941A1 (en) * | 2018-10-15 | 2021-04-29 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5464764A (en) | 1989-08-22 | 1995-11-07 | University Of Utah Research Foundation | Positive-negative selection methods and vectors |
| AU2515992A (en) | 1991-08-20 | 1993-03-16 | Genpharm International, Inc. | Gene targeting in animal cells using isogenic dna constructs |
| US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| WO2003091256A1 (en) * | 2002-04-23 | 2003-11-06 | Shionogi & Co., Ltd. | PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME |
| US7329662B2 (en) | 2003-10-03 | 2008-02-12 | Hoffmann-La Roche Inc. | Pyrazolo-pyridine |
| RU2412943C2 (en) * | 2005-03-23 | 2011-02-27 | Ф. Хоффманн-Ля Рош Аг | ACETYLENYL-PYRAZOLE-PYRIMIDINE DERIVATIVES AS mGluR2 ANTAGONISTS |
| JP5048675B2 (en) | 2005-09-27 | 2012-10-17 | エフ．ホフマン−ラ ロシュ アーゲー | Oxadiazolyl pyrazolo-pyrimidines as mGluR2 antagonists |
| JP4847275B2 (en) * | 2005-10-21 | 2011-12-28 | 田辺三菱製薬株式会社 | Pyrazolo [1,5-a] pyrimidine compounds |
| WO2008045664A2 (en) * | 2006-10-06 | 2008-04-17 | Kalypsys, Inc. | Heterocyclic pde4 inhibitors as antiinflammatory agents |
| KR20090075714A (en) * | 2006-10-30 | 2009-07-08 | 노파르티스 아게 | Heterocyclic compounds as antiinflammatory agents |
| AR067326A1 (en) | 2007-05-11 | 2009-10-07 | Novartis Ag | IMIDAZOPIRIDINES AND PIRROLO -PIRIMIDINES REPLACED AS INHIBITORS OF LIPIDO KINASE |
| ES2548135T3 (en) * | 2008-05-13 | 2015-10-14 | Novartis Ag | Condensed heterocycles containing nitrogen and compositions thereof as kinase inhibitors |
| TWI491610B (en) * | 2008-10-09 | 2015-07-11 | 必治妥美雅史谷比公司 | Imidazopyridazinecarbonitriles useful as kinase inhibitors |
| SG10201914059WA (en) * | 2008-10-22 | 2020-03-30 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
| BRPI1011066A2 (en) * | 2009-05-20 | 2017-03-21 | Cylene Pharmaceuticals Inc | "pyrazolopyrimidines and related heterocycles as kinase inhibitors |
| AR077468A1 (en) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | PIRAZOLO COMPOUNDS (1,5-A) PYRIMIDINE SUBSTITUTED AS TRK-QUINASA INHIBITORS |
| WO2011073316A1 (en) * | 2009-12-18 | 2011-06-23 | Novartis Ag | 4-aryl-butane-1,3-diamides |
| US8946237B2 (en) * | 2010-01-14 | 2015-02-03 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-A]pyrimidines as mark inhibitors |
| CN103748099B (en) * | 2011-05-19 | 2016-08-17 | 卡洛斯三世国家癌症研究中心基金会 | Macrocyclic compound as kinases inhibitor |
| ES2657061T3 (en) | 2012-03-09 | 2018-03-01 | Lexicon Pharmaceuticals, Inc. | Inhibition of kinase 1 associated with adapter for pain treatment |
| US8946415B2 (en) * | 2012-03-09 | 2015-02-03 | Lexicon Pharmaceuticals, Inc. | Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use |
| GB201205669D0 (en) * | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
-
2014
- 2014-09-02 TW TW103130281A patent/TW201542550A/en unknown
- 2014-09-03 AR ARP140103297A patent/AR097545A1/en unknown
- 2014-09-05 CA CA2923317A patent/CA2923317C/en active Active
- 2014-09-05 AU AU2014315113A patent/AU2014315113B2/en active Active
- 2014-09-05 US US14/478,089 patent/US20150175610A1/en not_active Abandoned
- 2014-09-05 CN CN201480049185.3A patent/CN105517553B/en active Active
- 2014-09-05 WO PCT/US2014/054209 patent/WO2015035117A1/en active Application Filing
- 2014-09-05 JP JP2016540405A patent/JP6472450B2/en active Active
- 2014-09-05 EP EP14766634.1A patent/EP3041475A1/en active Pending
-
2016
- 2016-05-03 US US15/145,435 patent/US9862724B2/en active Active
- 2016-05-20 HK HK16105787.8A patent/HK1217658A1/en unknown